Towa Pharmaceutical Co., Ltd., 26-7 Ichiban-Cho, Kadoma, Osaka 571-0033, Japan.
Int J Pharm. 2012 Feb 28;423(2):351-9. doi: 10.1016/j.ijpharm.2011.10.050. Epub 2011 Nov 26.
The aim of this study is to design a new orally disintegrating tablet (ODT) containing micronized ethylcellulose (MEC). The new ODT was prepared by physical mixing of rapidly disintegrating granules (RDGs) with MEC. To obtain RDGs, mannitol was spray-coated with a suspension of corn starch and crospovidone (9:1, w/w ratio) using a fluidized-bed granulator (suspension spray-coating method). The new ODTs were evaluated for their hardness, friability, thickness, internal structure (X-ray-CT scanning), in vivo disintegration time, and water absorption rate. Since MEC increases tablet hardness by increasing the contact frequency between the granules, the new ODTs could obtain high hardness (>50 N) and low friability (<0.5 %) with relatively low compression force. In addition, fine capillary channels formed in ODTs facilitated the wicking action and enabled rapid disintegration in vivo (<30 s). On the other hand, since MEC has low hygroscopicity, the tablet hardness of ODTs containing MEC remained high for 1 month in high-humidity conditions. In conclusion, the new ODTs containing MEC developed in this study possessed superior properties for clinical use and are expected to be applied for a wide range of functionally released drugs for bitter taste masking, sustained release, and controlled release (pH-dependent film coating, matrix, and microcapsule).
本研究旨在设计一种含有微粉化乙基纤维素（MEC）的新型口腔崩解片（ODT）。新型 ODT 通过将快速崩解颗粒（RDG）与 MEC 物理混合制备而成。为了获得 RDG，甘露醇采用流化床造粒机（悬浮喷雾涂层法）用玉米淀粉和交联聚维酮（9:1，w/w 比）混悬液喷雾包衣。对新型 ODT 的硬度、脆碎度、厚度、内部结构（X 射线计算机断层扫描）、体内崩解时间和吸水率进行了评估。由于 MEC 通过增加颗粒之间的接触频率来增加片剂的硬度，因此新型 ODT 可以在相对较低的压缩力下获得高硬度（>50N）和低脆碎度（<0.5%）。此外，ODT 中形成的精细毛细管通道促进了虹吸作用，使体内快速崩解（<30s）。另一方面，由于 MEC 的吸湿性低，在高湿度条件下，含有 MEC 的 ODT 的片剂硬度在 1 个月内仍保持较高水平。总之，本研究中开发的含有 MEC 的新型 ODT 具有优异的临床应用特性，有望应用于广泛的具有苦味掩蔽、缓释和控释功能的释放药物（pH 依赖性薄膜包衣、基质和微胶囊）。
